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WO2006060346A3 - 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists - Google Patents

8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists Download PDF

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Publication number
WO2006060346A3
WO2006060346A3 PCT/US2005/043002 US2005043002W WO2006060346A3 WO 2006060346 A3 WO2006060346 A3 WO 2006060346A3 US 2005043002 W US2005043002 W US 2005043002W WO 2006060346 A3 WO2006060346 A3 WO 2006060346A3
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WO
WIPO (PCT)
Prior art keywords
phenyl
receptor antagonists
hydroquinoline
tachykinin receptor
compounds
Prior art date
Application number
PCT/US2005/043002
Other languages
French (fr)
Other versions
WO2006060346A2 (en
Inventor
Jianming Bao
Robert J Devita
Jinlong Jiang
Sander G Mills
Original Assignee
Merck & Co Inc
Jianming Bao
Robert J Devita
Jinlong Jiang
Sander G Mills
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc, Jianming Bao, Robert J Devita, Jinlong Jiang, Sander G Mills filed Critical Merck & Co Inc
Priority to JP2007544424A priority Critical patent/JP2008521902A/en
Priority to CA002589639A priority patent/CA2589639A1/en
Priority to US11/667,908 priority patent/US20080039494A1/en
Priority to AU2005312076A priority patent/AU2005312076A1/en
Priority to EP05852331A priority patent/EP1819677A4/en
Publication of WO2006060346A2 publication Critical patent/WO2006060346A2/en
Publication of WO2006060346A3 publication Critical patent/WO2006060346A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Anesthesiology (AREA)
  • Nutrition Science (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

The present invention is directed to certain 8-phenyl-5,6,7,8-hydroquinolinecompounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
PCT/US2005/043002 2004-12-03 2005-11-29 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists WO2006060346A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2007544424A JP2008521902A (en) 2004-12-03 2005-11-29 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonist
CA002589639A CA2589639A1 (en) 2004-12-03 2005-11-29 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists
US11/667,908 US20080039494A1 (en) 2004-12-03 2005-11-29 8-Phenyl-5,6,7,8-Hydroquinoline Tachykinin Receptor Antagonists
AU2005312076A AU2005312076A1 (en) 2004-12-03 2005-11-29 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists
EP05852331A EP1819677A4 (en) 2004-12-03 2005-11-29 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63278904P 2004-12-03 2004-12-03
US60/632,789 2004-12-03

Publications (2)

Publication Number Publication Date
WO2006060346A2 WO2006060346A2 (en) 2006-06-08
WO2006060346A3 true WO2006060346A3 (en) 2006-11-16

Family

ID=36565608

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/043002 WO2006060346A2 (en) 2004-12-03 2005-11-29 8-phenyl-5,6,7,8-hydroquinoline tachykinin receptor antagonists

Country Status (7)

Country Link
US (1) US20080039494A1 (en)
EP (1) EP1819677A4 (en)
JP (1) JP2008521902A (en)
CN (1) CN101068787A (en)
AU (1) AU2005312076A1 (en)
CA (1) CA2589639A1 (en)
WO (1) WO2006060346A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1298717C (en) * 2000-12-22 2007-02-07 阿尔米雷尔普罗迪斯制药有限公司 Quinuclidine carbamate derivatives and their use as M3 antigonists
ES2246170B1 (en) * 2004-07-29 2007-04-01 Almirall Prodesfarma, S.A. NEW PROCEDURE TO PREPARE DERIVATIVES OF QUINUCLIDIN CARBAMATE.
US20080009518A1 (en) * 2004-12-03 2008-01-10 Jaime Bunda 5-Phenyl-5,6,7,8-Hydroquinoline Tachykinin Receptor Antagonists
EP2144503B9 (en) * 2007-04-10 2013-09-04 Merck Sharp & Dohme Corp. 4-(octahydro-2H-isoindol-2-yl)-1,3-oxazol-4-one as TACHYKININ RECEPTOR ANTAGONISTS
DE102008001932A1 (en) 2008-05-21 2009-11-26 Bayer Cropscience Ag Substituted spiroisoxazolines
ES2672099T3 (en) 2011-07-04 2018-06-12 Irbm - Science Park S.P.A. NK-1 receptor antagonists for the treatment of corneal neovascularization
US20210015834A1 (en) 2018-02-26 2021-01-21 Ospedale San Raffaele S.R.L. Nk-1 antagonists for use in the treatment of ocular pain
US20230134843A1 (en) 2020-03-11 2023-05-04 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998047874A1 (en) * 1997-04-22 1998-10-29 Janssen Pharmaceutica N.V. Crf antagonistic quino- and quinazolines

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998047874A1 (en) * 1997-04-22 1998-10-29 Janssen Pharmaceutica N.V. Crf antagonistic quino- and quinazolines

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
HUANG ET AL.: "Synthesis and SAR of 8-Arylquinolines as Potent Corticotropin-Releasing Factor1 (CRF1) Receptor Antagonists", BIOORG. MED. CHEM. LETT., vol. 13, March 2003 (2003-03-01), pages 3375 - 3379, XP003001897 *
KATSUJI ET AL.: "Chiral Bipyridine and Biquinoline Ligands: Their Asymmetric Synthesis and Application to the Synthesis of trans-Whisky Lactone tetrahedron", vol. 52, no. 11, 1996, pages 3905 - 3920, XP004196624 *
See also references of EP1819677A4 *

Also Published As

Publication number Publication date
US20080039494A1 (en) 2008-02-14
AU2005312076A1 (en) 2006-06-08
JP2008521902A (en) 2008-06-26
CN101068787A (en) 2007-11-07
WO2006060346A2 (en) 2006-06-08
CA2589639A1 (en) 2006-06-08
EP1819677A4 (en) 2009-03-11
EP1819677A2 (en) 2007-08-22

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